Title
New salicylamide and sulfonamide derivatives of quinoxaline 1,4-di-N-oxide with antileishmanial and antimalarial activities
Date Issued
01 August 2011
Access level
open access
Resource Type
journal article
Author(s)
Barea C.
Pabón A.
Galiano S.
Pérez-Silanes S.
Monge A.
Deharo E.
Aldana I.
Universidad Peruana Cayetano Heredia
Universidad Peruana Cayetano Heredia
Universidad Peruana Cayetano Heredia
Abstract
Continuing with our efforts to identify new active compounds against malaria and leishmaniasis, 14 new 3-amino-1,4-di-N-oxide quinoxaline-2- carbonitrile derivatives were synthesized and evaluated for their in vitro antimalarial and antileishmanial activity against Plasmodium falciparum Colombian FCR-3 strain and Leishmania amazonensis strain MHOM/BR/76/LTB-012A. Further computational studies were carried out in order to analyze graphic SAR and ADME properties. The results obtained indicate that compounds with one halogenous group substituted in position 6 and 7 provide an efficient approach for further development of antimalarial and antileishmanial agents. In addition, interesting ADME properties were found. © 2011 Elsevier Ltd. All rights reserved.
Start page
4498
End page
4502
Volume
21
Issue
15
Language
English
OCDE Knowledge area
Enfermedades infecciosas
Subjects
Scopus EID
2-s2.0-79960341464
PubMed ID
Source
Bioorganic and Medicinal Chemistry Letters
ISSN of the container
0960894X
Sources of information:
Directorio de Producción Científica
Scopus